A sensitive, rapid and specific liquid chromatographic-tandem mass spectrometric (LC-MS/MS) method for quantification of gabapentin in human plasma has been developed. After a single plasma protein precipitation with methanol, gabapentin and metformin (internal standard) were chromatographed on a Inertsil ODS-3 column (50 mm x 2.1 mm ID, 3 microm) with mobile phase consisting of methanol-0.2% formic acid aqueous solution (80:20, v/v) at a flow-rate of 0.2 mL x min(-1). Electrospray ionization (ESI) source was applied and operated in the positive ion mode. Multiple reaction monitoring (MRM) mode with the transitions of m/z 172 --> m/z 154 and m/z 130 --> m/z 71 were used to quantify gabapentin and metformin, respectively. The run time was 2.2 min. The linear calibration curve was obtained in the concentration range of 40.8-8.16x10(3) ng x mL(-1). The lower limit of quantification was 40.8 ng x mL(-1). The intra- and inter-day precision (RSD) was less than 12%, and the accuracy (RE) was within +/-6.4% calculated from quality control (QC) samples. The method was used to determine the concentration of gabapentin in human plasma after a single oral administration of 600 mg gabapentin capsule to 20 healthy male Chinese volunteers. The method was proved to be selective, sensitive, rapid and suitable for pharmacokinetic study of gabapentin in human plasma.

Orally disintegrating tablets (ODT), a kind of new solid tablet that rapidly disintegrates to work in the mouth, has became the hot form of new drug research in recent years with many advantages, such as the convenient taking, a widely applicable people, fast acting, high bioavailability, good compliance, and so on. ODT has been widely used in chemical medicines, while the application of it in traditional Chinese medicines (TCMs) is still in the stage of development The development of TCMs ODT provides a new direction for the research of Chinese medicine new dosage, accelerates the pace of connecting to the world and modernization of Chinese medicine. This dosage has a broad market prospect, and its quality control and assessment standards, taste, the disintegration time in vitro and evaluation method are the key factors that affect the industrialization, standardization of Chinese medicine ODT. Therefore, this paper reviewed the characteristics, preparation, taste masking technology and quality evaluation with new technology of ODT. Meantime, numerous application examples of ODT used in traditional Chinese medicine were described. We expect to provide the reference and utilization for the development of traditional Chinese medicine orally disinteeratine tablets.
Administration, Oral ; Drug Compounding ; methods ; Humans ; Medicine, Chinese Traditional ; Solubility ; Tablets ; administration & dosage ; chemistry ; Taste

Objective To explore the clinical and neuroimaging features of a frontotemporal dementia with parkinsonism linked to chromosome 17 ( FTDP-17 ) pedigree caused by mutation of microtubule-associated protein tau ( MAPT) gene.Methods The proband and one patient from a FTDP-17 pedigree were assessed through standardized clinical evaluation , neuropsychology assessment , video-electroencephalogrom ,MRI, genetic sequencing , as well as 18 F fludeoxyglucose ( FDG) SPECT for brain metabolism and 11 C 2β-carbomethoxy-3β-( 4-fluoro ) tropane ( CFT ) PET for dopamine transporter ( DAT ) distribution, respectively.Results A FTDP pedigree with 15 patients (6 still alive) was recruited to this study.The proband and one affected patient were genotyped and confirmed as MAPT c .1788T>G mutation. Parkinsonism was the first symptom for both two patients . Personality, speech changes and dementia accompanied with brain atrophy were developed at the later stage in one patient .The 18 F FDG SPECT studies illustrated asymmetric hypometabolism of the temporal , frontal lobes and basal ganglia in two patients . Regarding to the 11 C CFT PET, one affected patient showed asymmetric decreased uptake of tracer in basal ganglia regions.Conclusions FTDP-17 can display a confusingly broad clinical phenotype , with the parkinsonism as the first symptom . Brain glucose metabolism and DAT distribution could be potential biomarkers in early diagnosis of FTDP-17.

The study on the pharmacokinetics of traditional Chinese medicines (TCMs) is a linking science during the modernization of TCMs, and plays an important role in the studies on the complex material base of TCMs, the in vivo process of ingredient/ component and the pharmacokinetics-pharmacodynamics correlation. However, because of the multi-ingredient/component system of TCMs, how to scientifically reveal the pharmacokinetics that is consistent with TCMs' characteristics has long been a hotspot and difficulty for the exploration. The optimal composition structure of the material basis of TCMs shows the best efficacy, while the difference between the multi-ingredient/component composition structures in the efficacy is closely related to their absorption, transport, metabolism and excretion in vivo. In this article, the authors systematically review the study methods for pharmacokinetics of TCMs and their compounds, and explore the pharmacokinetics of TCMs based on the "component structure theory". As a result, the method for integrating TCM component structure and the TCM pharmacokinetics was proposed to be adopted to intensively study the effect of the component structure on the in vivo TCM multi-ingredient/component pharmacokinetic characteristics, in order to promote the TCM modernization and innovation in China.
Animals ; Area Under Curve ; Chemistry, Pharmaceutical ; Humans ; Medicine, Chinese Traditional ; methods ; Pharmacokinetics ; Structure-Activity Relationship

OBJECTIVETo explore the clinical effects of Mobi-C cervical artificial disc replacement (CADR) and anterior cervical decompression and fusion (ACDF) in treating single cervical disc herniation.

METHODSFrom June 2009 to June 2012, the clinical data of 27 patients with single cervical disc herniation were retrospectively analyzed. There were 18 males and 9 females, aged from 30 to 62 years old with an average of 46.7 years. Of them, 12 patients were treated with CADR (CADR group) and 15 patients with ACDF (ACDF group). All patients had pain and numbness in neck, shoulder and upper limbs, and courses of disease was from 1 to 13 months with an average of 2.4 months. The data of clinical evaluation and questionnaire survey about quality of life were collected before operation, postoperative at 1 week and final follow-up. Odom criterion was used to evaluate postoperative effect. Visual analogue scale (VAS) was used to record pain levels. Neck disability index (NDI) and health questionnaire SF-36 were used to assess the quality of life.

RESULTSNo complications about nerve and blood vessel were found and the patients were followed up from 6 to 30 months, with an average of 16 months. One week after operation, 10 cases got excellent results and 2 good in CADR group; 5 cases got excellent results and 10 good in ACDF group; there was significant difference between two groups (P<0.05). At final follow-up, 10 cases got excellent results and 2 good in CADR group; 12 cases got excellent results and 3 good in ACDF group; there was no significant difference between two groups (P> 0.05). Pain of upper limbs had obviously relieved between two groups at 1 week after operation and final follow-up (P<0.05). VAS of neck and NDI in CADR group had decreased respectively from preoperative 3.58±0.79, 23.42±6.36 to 0.58±0.51, 5.42±1.68 at 1 week after operation (P<0.05); but the index in ACDF group was no obvious at 1 week after operation. At final follow-up, VAS of neck and NDI and SF-36 score were obviously improved than preoperation (P<0.05) between two groups.

CONCLUSIONMobi-C CADR retains the movement unit in the decompression segment and can quickly recover normal action for patients. Using CADR method has a good curative effect in the early phase, and the clinical effect is reliable, may improve the quality of life.

Adult ; Decompression, Surgical ; methods ; Female ; Humans ; Intervertebral Disc Displacement ; surgery ; Male ; Middle Aged ; Retrospective Studies ; Spinal Fusion ; methods ; Total Disc Replacement ; methods ; Visual Analog Scale

OBJECTIVETo investigate the effects of hydrogen sulfide (H₂S) on oxidative stress and endoplasmic reticulum stress (ERS) in a rat model of diabetic cardiomyopathy (DCM).

METHODSThirty male SD rats were randomly divided into control group, diabetes group and treatment group( n = 10). Intraperitoneal injection of streptozotocin was utilized to establish a rat model of DCM. The rats with DCM in treatment group were intraperitoneally injected with NaHS solution. After treated for 12 weeks, the hearts isolated from rats were perfused on a langendorff apparatus. The ventricular hemodynamic parameters were measured. The ultrastructures of myocardium were observed using electron microscopy. The content of malondialdehyde (MDA), the activities of superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) in myocardial tissue were determined by spectrophotometry. The expressions of C/EBP homologous protein( CHOP), glucose-regulated protein 78 (GRP78) and Caspase 12 at mRNA level in myocardium were detected using RT-PCR.

RESULTSCompared with control group, the cardiac function and myocardial ultrastructure were damaged obviously in diabetic rats. In myocardial tissue, the content of MDA was increased, while the activities of SOD and GSH-Px were decreased. CHOP, GRP78 and Caspase 12 mRNA expressions were increased significantly. Compared with diabetes group, cardiac function and myocardial ultrastructure damage were improved in treatment group. The content of MDA was decreased, while the activities of SOD and GSH-Px were increased significantly. The mRNA levels of CHOP, GRP78 and Caspase 12 were increased.

CONCLUSIONH2S can protect myocardium in diabetic rats, maybe it is related to reduce oxidative stress damage and inhibition of the ERS-induced apoptosis pathway.

Animals ; Apoptosis ; Caspase 12 ; metabolism ; Diabetes Mellitus, Experimental ; drug therapy ; Diabetic Cardiomyopathies ; drug therapy ; Endoplasmic Reticulum Stress ; Glutathione Peroxidase ; metabolism ; Heat-Shock Proteins ; metabolism ; Hydrogen Sulfide ; pharmacology ; Male ; Malondialdehyde ; metabolism ; Myocardium ; ultrastructure ; Oxidative Stress ; Rats ; Streptozocin ; Superoxide Dismutase ; metabolism ; Transcription Factor CHOP ; metabolism

Objective To assess the efficacy of combination of Jiehe pellet and the standardized anti-tuberculosis therapeutic regimen for pulmonary tuberculosis complicating cervical lymph node tuberculosis in the aged. Methods A total of 103 aged patients with pulmonary tuberculosis complicating cervical lymph node tuberculosis were enrolled and randomly allocated to either a standardized anti-tuberculosis therapeutic regimen group (control group with 51 patients) or a standardized anti-tuberculosis therapeutic regimen plus Jiehe pellet group (treatment group with 52 patients). The patients in the control group and the treatment group received the treatment with 2HRZE/4HR and 2HRZE/4HR plus Jiehe pellet for 6 months, respectively. The abscessed lymph nodes were treated by either total excision or incision and drainage after 4 weeks of medicine treatment in both groups. Sputum smear was examined for acid-fast bacilli. The CD8 cells expressing natural killer T cells receptors NKG2A, NKG2D in peripheral blood were detected by flow cytometry. The treatment outcome was measured at the end of treatment. Results The rates of lesion resolution (78.85%vs. 58.82%;χ2=4.439, P<0.05) and cavity closure (62.86% vs. 35.48%;χ2=3.893, P<0.05) in the treatment group were significantly higher than those in the control group. In the end of 2, 4 and 6 months of treatment, cumulative rates of sputum conversion from positive to negative in the treatment group were significantly higher than those in the control group (χ2 were 5.343, 5.067 and 4.118,all P<0.05). The CD8 cells expressing NKG2A after treatment in the treatment group were significantly lower than those before treatment in the treatment group (t=9.510, P<0.01) and after treatment in the control group (t=9.832, P<0.01);the CD8 cells expressing NKG2D after treatment in the treatment group were significantly higher than those before treatment in the treatment group (t=10.622, P<0.01) and after treatment in the control group (t=10.433, P<0.01). The serum levels of IL-6 and TNF-αafter treatment were significantly lower than those before treatment in both groups (t were 17.344 and 21.142 in the treatment group, 10.984 and 12.203 in the control group;all P<0.01 );the serum levels of IL-6 and TNF-α after treatment in the treatment group were significantly lower than those after treatment in the control group (t were 7.832 and 5.478,all P<0.01). The serum IL-10 levels after treatment were significantly higher than those before treatment in both groups (t were 12.454 in the treatment group, 7.934 in the control group; all P<0.01 ); and the serum IL-10 level after treatment in the treatment group was significantly higher than that after treatment in the control group (t=4.720, P<0.01). The effective rate for cervical lymph node tuberculosis in the treatment was significantly higher than that in the control group (88.5%vs. 64.7%;χ2=6.855, P<0.01). Conclusion Combination of Jiehe pellet and the standardized anti-tuberculosis therapeutic regimen may improve immune function, increase the rate of sputum conversion from positive to negative, and facilitate lesion resolution in aged patients with pulmonary tuberculosis complicating cervical lymph node tuberculosis.

Objective To explore the characteristics and data collection sources of featured literature databases in universities/colleges in Yunnan in order to provide evidence for building featured literature databases. Methods Key information about three types of featured literature databases was retrieved online, which included those being constructed jointly by some universities or colleges in Yunnan, owned by universities or colleges in Yunnan, and already in use in China Academic Library and Information System ( CALIS) , respectively. Comparison was performed among these featured literature databases in regard to data characteristics and collection sources. Results Among all the featured databases being constructed, 58.8% were based on literature on local resources, 17.6% on disciplines and specialties, and 11.8% on library literature. In-use featured databases in Yunnan were mainly based on local resources and disciplines, and the data were collected within their own organizations or through multi-sources. The featured databases in CALIS were of local resources, disciplines, and people, while their data were collected mainly within their own organizations, through other organizations and multi-sources. Conclusion Yunnan featured databases are of unique characteristics, but more should be done to define Yunnan style data, while it is necessary to collect data from a wider range of sources.

AIM:To observe the structural basis of ocular motility abnormalities in patients with congenital fibrosis of the extraocular muscles type Ⅰ ( CFEOM Ⅰ) due to missense mutations in the developmental kinesin KIF21A using high - resolution magnetic resonance imaging ( MRI) .
METHODS: Totally 11 affected individuals reported KIF21A mutations were correlated with MRI studies demonstrating extraocular muscles ( EOMs ) size, location, contractility, and innervation. EOMs and the motor nerve in the orbits were imaged with T1 weighted in a triplanar scan using a dual-phased coils with 2. 0mm thick. Motor nerves were imaged at the brainstem using head coils and 3D-FIESTA with 0. 6-mm thick.
RESULTS: Patients with CFEOM Ⅰ exhibited different degrees of hypoplasia of oculomotor nerve, the abducens nerve and the trochlear nerve were also affected, of which 8 cases of orbital section could see the signal of abnormal nerve dominated by oculomotor nerve to lateral rectus. The both sides of six EOMS in all patients exhibited variable atrophy and abnormal bright internal signal on T1 imaging, particularly severe for the superior rectus and levator muscles.
CONCLUSION: High - resolution MRI can directly demonstrate pathology of motor nerves,affected EOMs, and ‘Pulley' hypoplasia caused by CFEOM Ⅰ due to mutations in KIF21A,and these findings suggest that the neuronal hypoplasia is the etiological factor of CFEOM.

Objective To investigate the changes and significance of concentration of soluble intercellular adhesion molecule-1(sICAM-1) in cerebrospinal fluid (CSF) of bacterial meningitis(BM) in rabbits. Methods A total of 36 rabbits were randomly divided into m eningitis group, meningitis cefotaxime-treated group and control group. BM indu ced by escherichia coli(Ec) via cerebellomedullary cistern inoculated. Normal sa line was injected in control group. CSF was sampled in different time. The conce ntration of CSF sICAM-1 was detected by ELISA.Results 1.There was a low concentration of sICAM-1 in CSF in 85 percent of normal rabbi ts.2.In meningitis group, there was a sharp rise in the concentration of CSF sIC AM-1 at 6 hours after Ec was inoculated, reached a peak level at 12 hours, and t here was higher concentration of CSF sICAM-1 between 6 and 24 hour than that at 0 hour.3.In meningitis cefotaxime-treated group, the concentration of CSF sICAM -1 at 6 hour and 12 hours was similar to meningitis group, the time that get pe ak level was at 24 hours that at 12 hours after making use of antimicrobial agen t.The peak level was higher than meningitis group. The concentration of CSF sICA M-1 decreased markedly at 48 hours that made use of antimicrobial agent 36 hour s later,but the concentration was still higher than the peak level of meningitis group.Afterwards, with the time of making use of antimicrobial agent lengthened ,the concentration of CSF sICAM-1 decreased gradually.4.Experimental results in dicated by correlating analysis to these data that there was positive correlatio n in the concentration of CSF sICAM-1 with the brain water content.Conclusions sICAM-1 participates in the pathological process of BM, and contributes to the damage of blood brain barrier and the formation of brain edema.There is importan t significance that drugs which can resist the discharge of sICAM-1 will be impl ied. J Appl Clin Pediatr,2005,20(2):163-165